Dimethylformamide → HCID 71009175, compound

Participants

Reaction Steps

A mixture of (R)-4-(1-(3-bromophenyl)-1H-pyrazol-4-yl)-5,5-difluoro-4-methyl-5,6-dihydro-4H-1,3-oxazin-2-amine (20 mg, 53.9 μmol) (intermediate K7.1), zinc cyanide (3.8 mg, 32.3 μmol) and tetrakis(triphenylphosphine)-palladium(0) (6.23 mg, 5.39 μmol) was heated at 160° C. in N,N-dimethylformamide (0.5 ml) for 30 minutes in a microwave oven. Thereafter, the reaction mixture was evaporated at reduced pressure and purified by preparative HPLC. The 3-[4-((R)-2-amino-5,5-difluoro-4-methyl-5,6-dihydro-4H-[1,3]oxazin-4-yl)-pyrazol-1-yl]-benzonitrile (79% yield) was obtained as a light brown solid. MS (ISP): m/z=318.1 [M+H]+.

Provenance & Evidence